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Assay Detail

CHEMBL3370677

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Gong H, Yang M, Xiao Z, Doweyko AM, Cunningham M, Wang J, Habte S, Holloway D, Burke C, Shuster D, Gao L, Carman J, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS.
Bioorg Med Chem Lett (2014) 24 : 3268 -3273
PubMed 24980053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.40 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3315064 1 9.15
CHEMBL3315070 1 9.15
CHEMBL384467 DEXAMETHASONE 4.0 1 8.92
CHEMBL3315066 1 8.92
CHEMBL3315063 1 8.82
CHEMBL3315049 1 8.80
CHEMBL3315062 1 8.80
CHEMBL1911270 1 8.72
CHEMBL3315065 1 8.72
CHEMBL3315067 1 8.70
CHEMBL3315061 1 8.68
CHEMBL3315051 1 8.60
CHEMBL3315069 1 8.40
CHEMBL3315058 1 8.24
CHEMBL3315052 1 8.23
CHEMBL3315057 1 8.16
CHEMBL3315068 1 8.14
CHEMBL3315060 1 8.13
CHEMBL3315054 1 8.07
CHEMBL3315059 1 8.06
CHEMBL3315055 1 8.06
CHEMBL3315053 1 7.89
CHEMBL3315050 1 7.16
CHEMBL3315056 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3315064 Ki = 0.7 nM 9.15
CHEMBL3315070 Ki = 0.7 nM 9.15
CHEMBL384467 DEXAMETHASONE Ki = 1.2 nM 8.92
CHEMBL3315066 Ki = 1.2 nM 8.92
CHEMBL3315063 Ki = 1.5 nM 8.82
CHEMBL3315049 Ki = 1.6 nM 8.80
CHEMBL3315062 Ki = 1.6 nM 8.80
CHEMBL1911270 Ki = 1.9 nM 8.72
CHEMBL3315065 Ki = 1.9 nM 8.72
CHEMBL3315067 Ki = 2.0 nM 8.70
CHEMBL3315061 Ki = 2.1 nM 8.68
CHEMBL3315051 Ki = 2.5 nM 8.60
CHEMBL3315069 Ki = 4.0 nM 8.40
CHEMBL3315058 Ki = 5.7 nM 8.24
CHEMBL3315052 Ki = 5.9 nM 8.23
CHEMBL3315057 Ki = 6.9 nM 8.16
CHEMBL3315068 Ki = 7.3 nM 8.14
CHEMBL3315060 Ki = 7.4 nM 8.13
CHEMBL3315054 Ki = 8.5 nM 8.07
CHEMBL3315059 Ki = 8.7 nM 8.06
CHEMBL3315055 Ki = 8.7 nM 8.06
CHEMBL3315053 Ki = 12.9 nM 7.89
CHEMBL3315050 Ki = 69.4 nM 7.16
CHEMBL3315056 Ki = 110.5 nM 6.96